Verma Shristy, Sharma Pramod Kumar, Malviya Rishabha
Department of Pharmacy, School of Medical and Allied Sciences, Galgotias University, Greater Noida, Uttar Pradesh, India.
Curr Drug Deliv. 2025;22(6):678-693. doi: 10.2174/0115672018285350240227073607.
The intricate anatomical and physiological barriers that prohibit pharmaceuticals from entering the brain continue to provide a noteworthy hurdle to the efficient distribution of medications to brain tissues. These barriers prevent the movement of active therapeutic agents into the brain. The present manuscript aims to describe the various aspects of brain-targeted drug delivery through the nasal route. The primary transport mechanism for drug absorption from the nose to the brain is the paracellular/extracellular mechanism, which allows for rapid drug transfer. The transcellular/intracellular pathway involves the transfer across a lipoidal channel, which regulates the entry or exit of anions, organic cations, and peptides. Spectroscopy and PET (positron emission tomography) are two common methods used for assessing drug distribution. MRI (Magnetic resonance imaging) is another imaging method used to assess the efficacy of aerosol drug delivery from nose to brain. It can identify emphysema, drug-induced harm, mucus discharge, oedema, and vascular remodeling. The olfactory epithelium's position in the nasal cavity makes it difficult for drugs to reach the desired target. Bi-directional aerosol systems and tools like the "OptiNose" can help decrease extranasal particle deposition and increase particle deposition efficiency in the primary nasal pathway. Direct medicine administration from N-T-B, however, can reduce the dose administered and make it easier to attain an effective concentration at the site of activity, and it has the potential to be commercialized.
阻碍药物进入大脑的复杂解剖学和生理学屏障,仍然是药物有效分布到脑组织的一个显著障碍。这些屏障阻止活性治疗药物进入大脑。本手稿旨在描述经鼻途径进行脑靶向给药的各个方面。药物从鼻腔吸收到大脑的主要转运机制是细胞旁/细胞外机制,它允许药物快速转移。跨细胞/细胞内途径涉及通过脂质通道的转移,该通道调节阴离子、有机阳离子和肽的进出。光谱学和正电子发射断层扫描(PET)是用于评估药物分布的两种常用方法。磁共振成像(MRI)是另一种用于评估从鼻腔到大脑的气溶胶药物递送效果的成像方法。它可以识别肺气肿、药物引起的损伤、黏液分泌、水肿和血管重塑。嗅上皮在鼻腔中的位置使得药物难以到达期望的靶点。双向气溶胶系统和诸如“OptiNose”之类的工具可以帮助减少鼻外颗粒沉积,并提高在主要鼻腔途径中的颗粒沉积效率。然而,从鼻到脑的直接药物给药可以减少给药剂量,并更容易在活性部位达到有效浓度,并且它具有商业化的潜力。